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Voxtalisib

Catalog No. T7014 CAS 934493-76-2

Synonyms: SAR245409, XL765

Voxtalisib (SAR245409, XL765) is a dual inhibitor of <a href="/target/mTOR" style="display: inline; color: #c13a36">mTOR</a>/<a href="/target/PI3K" style="display: inline; color: #c13a36">PI3K</a>, mostly for p110γ with IC50 of 9 nM; also inhibits <a href="/target/DNA_PK" style="display: inline; color: #c13a36">DNA-PK</a> and <a href="/target/mTOR" style="display: inline; color: #c13a36">mTOR</a>. Phase 1/2.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

Voxtalisib, CAS 934493-76-2

Pack Size	Availability	Price/USD
2 mg	In stock	$ 50.00
5 mg	In stock	$ 72.00
10 mg	In stock	$ 126.00
25 mg	In stock	$ 252.00
50 mg	In stock	$ 405.00
1 mL * 10 mM (in DMSO)	In stock	$ 72.00

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Purity: 99.24%

Purity: 99.36%

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Description	Voxtalisib (SAR245409, XL765) is a dual inhibitor of mTOR/PI3K, mostly for p110γ with IC50 of 9 nM; also inhibits DNA-PK and mTOR. Phase 1/2.
Targets&IC50	p110γ:9 nM
In vitro	XL765 is active against class I PI3K (IC50 = 39, 113, 9 and 43 nM for p110α, β, γ and δ, respectively). XL765 also inhibits DNA-PK (IC50 = 150 nM) and mTOR (IC50 = 157 nM) but not XL-147 which shows IC50 values of > 15 μM. [1] XL765 treatment results in decreased cell viability in 13 PDA cell lines in a dose-dependent manner. XL765, a dual-target PI3K/mTOR inhibitor, inhibits cell growth and apoptosis in many more cell lines and at lower concentrations as compared to the PI3K-selective inhibitors XL147 and PIK90. The effect can be recapitulated by using combinations of single-targeted compounds. XL765 significantly reduces phosphorylation of the mTOR targets S6, S6K, and 4EBP1, which is associated with greater apoptosis induction rather than to PI3K inhibition alone. XL765 treatment causes accumulation of autophagosomes in MIAPaCa-2 cells, and results in significant dose-dependent AVO induction and LC3-II stimulation in MIAPaCa-2 cells stably expressing a LC3-GFP construct. [2]
In vivo	The combination of XL765 (30 mg/kg) with chloroquine (50 mg/kg) results in significant inhibition of BxPC-3 xenograft growth in mice models, while XL765 alone at the same dose has no inhibitory effect. [2] Oral administration of XL765 results in greater than 12-fold reduction in median tumor bioluminescence compared to control and improvement in median survival in nude mice implanted intracranially with GBM 39-luc cells. XL765 in combination with temozolomide (TMZ) yields a 140-fold reduction in median bioluminescence with a trend toward improvement in median survival compared with TMZ alone. [3]
Cell Research	Cells are treated with XL765 24 hours after plating and harvested for apoptosis or autophagy assays at 24, 48, or 72 hours after XL765 treatment. Apoptosis is determined by total percentage of annexin V-positive cells by fluorescence-activated cell sorting (FACS). Acidic vesicular organelles (AVOs) are detected in XL765-treated cells by vital staining with acridine orange. The degree of AVO formation is expressed as fold increase of acridine orange fluorescence intensity (FL3) in XL765-treated cells versus control cells. (Only for Reference)

Synonyms	SAR245409, XL765
Molecular Weight	270.296
Formula	C13H14N6O
CAS No.	934493-76-2

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

Ethanol: <1 mg/mL

DMSO: 50 mg/mL (185 mM)

H2O: <1 mg/mL

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. Garcia-Echeverria C, et al. Oncogene, 2008, 27(41), 5511-5526. 2. Mirzoeva OK, et al. J Mol Med, 2011, 89(9), 877-889. 3. Prasad G, et al. Neuro Oncol, 2011, 13(4), 384-392.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Drug Library Anti-Prostate Cancer Compound Library Anti-Cancer Active Compound Library Human Metabolite Library Metabolism Compound Library Bioactive Compound Library Bioactive Compounds Library Max PI3K-AKT-mTOR Compound Library Anti-Cancer Metabolism Compound Library Glutamine Metabolism Compound Library

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NVP-BAG956 Niazimicin Isoangustone A Cimiside E Sennidin A Dehydroglyasperin D Sonolisib PI3Kα/mTOR-IN-1

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Keywords

Voxtalisib 934493-76-2 DNA Damage/DNA Repair PI3K/Akt/mTOR signaling PI3K DNA-PK mTOR SAR-245409 SAR 245409 SAR245409 inhibit Phosphoinositide 3-kinase Mammalian target of Rapamycin XL 765 Inhibitor XL765 XL-765 inhibitor

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